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1.
J Pers Med ; 14(5)2024 Apr 29.
Artigo em Inglês | MEDLINE | ID: mdl-38793052

RESUMO

The primary goal of this study was to investigate the knowledge, prevalence, and risk factors of cardiovascular diseases among individuals in the Najran region of Saudi Arabia. In the Najran region of Saudi Arabia, an online cross-sectional survey was conducted. Between September and October 2023, a self-administered questionnaire was distributed to a random sample of the general population aged 18 and up. The survey instrument asked about history and exposure, physician-diagnosed illnesses, cardiovascular diseases (CVDs), medication use, and other risk factors. This research had a total of 2046 individuals. Around one-fifth of the study participants reported that they or a family member suffered from CVD, and arrhythmia was the most commonly reported; blood tests, cardiac catheterization, and ECG were the most commonly reported tests performed for CVD patients, around one-tenth of CVD patients reported that they do not have any chronic diseases other than CVD, and the vast majority of the patients confirmed their regular medical appointments. This is one of the first studies to investigate the knowledge, prevalence, and use of CVD drugs among individuals in the Najran region of Saudi Arabia. The study participants' lack of knowledge about CVD could lead to ineffective preventive measures and poor patient outcomes. The study's findings underscore the crucial need for more extensive and efficient educational initiatives that consider the targeted population's talents, attitudes, and perceptions.

2.
ADMET DMPK ; 12(1): 167-176, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38560714

RESUMO

Background and purpose: Doxazosin mesylate (DOX) is an antihypertensive drug that possesses poor water solubility and, hence, poor release properties. Both nanosuspensions and self-nanoemulsifying drug delivery systems (SNEDDS) are becoming nanotechnology techniques for the enhancement of water solubility of different drugs. Experimental approach: The study's goal was to identify the best drug delivery system able to enhance the release and antihypertensive effect of DOX by comparing the physical characteristics such as particle size, zeta potential, entrapment efficiency, release rate, and main arterial blood pressure of DOX-loaded nanosuspensions and SNEDDS in liquid and solid form. Key results: DOX nanosuspension preparation had a particle size of 385±13 nm, poly-dispersity index of 0.049±3, zeta potential of 50 ± 4 mV and drug release after 20 min (91±0.43 %). Liquid SNEDDS had a droplet size of 224±15 nm, poly-dispersity index of (0.470±0.01), zeta potential of -5±0.10 mV and DR20min of 93±4 %. Solid SEDDS showed particle size of 79±14 nm, poly-dispersity index of 1±0.00, a zeta potential of -18 ±0.26 mv and DR20min of 100 ±2.72 %. Conclusion: Finally, in terms of the mean arterial blood pressure lowering, solid SNEDDS performed better effect than both liquid SNEDDS and nanosuspension (P >0.05).

3.
Saudi Pharm J ; 32(3): 101968, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38352238

RESUMO

Asthma is a chronic disease affecting people of all ages. Asthma medications are associated with adverse effects restricting their long-term usage, demanding newer alternative therapies. This study aimed to investigate the anti-asthmatic properties of Ruta graveolens extract and its prepared nano-cubosomal dispersion (Ruta-ND). Firstly, the R. graveolens methanolic extract exhibited higher anti-inflammatory activity on Lipopolysaccharide (LPS)-activated BEAS-2B cells. To ensure best bioavailability and hence best cellular uptake, R. graveolens extract was loaded in nano-cubosomal dispersion (ND). Then, the anti-asthmatic effects of Ruta extract and ND were simultaneously evaluated in rats' model with ovalbumin-induced allergic asthma. R. graveolens extract and Ruta-ND subsided asthma score and improved lung function by restoring FEV1/FVC ratio to the expected values in control rats. Also, it showed strong antioxidant and anti-inflammatory activities manifested by lowering levels of malondialdehyde (MDA), IL-4, IL-7, TGF-ß, and Ig-E, and increasing levels of superoxide dismutase (SOD) and INF-γ in bronchoalveolar lavage fluid. Our research findings also indicate autophagy induction and apoptosis inhibition by Ruta extract and Ruta-ND. Finally, the HPLC MS/MS phytochemical profiling of R. graveolens extract evident production of various alkaloids, flavonoids, coumarins, and other phenolics with reported pharmacological properties corresponding to/emphasize our study findings. In conclusion, R. graveolens exhibited promise in managing Ova-induced allergic asthma and could be developed as an alternative anti-allergic asthma drug.

4.
Gels ; 9(12)2023 Nov 25.
Artigo em Inglês | MEDLINE | ID: mdl-38131915

RESUMO

The purpose of this work was to develop a novel topical formulation of econazole nitrate based on gel that can be easily scaled up in one pot for the potential treatment of fungal and yeast infections. Econazole nitrate, a topical antifungal, is used to treat tinea versicolor, tinea pedis, and tinea cruris. Compared to applying cream or ointment, topical gels offer numerous advantages, one of which is that the drug is released more quickly to the intended site of action. A viscous mixture of propylene glycol, Capmul® MCM C8, methyl and propyl paraben, and econazole nitrate were mixed together before being formulated into the optimized Carbopol® gel bases. The gel's color, appearance, and homogeneity were assessed visually. For every formulation, the drug content, pH, viscosity, spreadability, and gel strength were characterized. The cup plate diffusion method was used to evaluate the anti-fungal activity of the prepared formulations. To assess the behavior of the developed system, studies on in vitro release and mechanism were conducted. The manufactured formulations were transparent, pale yellow, and exhibited excellent homogeneity. The pH of each formulation was roughly 6.0, making them suitable for topical use. The concentration of Carbopol® 940 resulted in a significant increase in viscosity and gel strength but a significant decrease in spreadability. It was demonstrated that the prepared formulations inhibited the growth of Candida albicans and Aspergillus fumigatus. In contrast, the standard blank gel showed no signs of antifungal action. By increasing the concentration of Carbopol® 940, the in vitro release profile of econazole nitrate significantly decreased. Following the Korsmeyer-Peppas model fitting, all formulations exhibited n values greater than 0.5 and less than 1, indicating that diffusion and gel swelling control econazole nitrate release.

5.
Pharmaceutics ; 15(12)2023 Nov 26.
Artigo em Inglês | MEDLINE | ID: mdl-38140018

RESUMO

Targeted drug delivery is achieving great success in cancer therapy due to its potential to deliver drugs directly to the action site. Terbinafine hydrochloride (TER) is a broad-spectrum anti-fungal drug that has been found to have some potential anti-tumor effects in the treatment of colon cancer. We aimed here to design and develop pH-sensitive Eudragit (Eud)-coated mesoporous silica nanostructures (MSNs) to control drug release in response to changes in pH. The diffusion-supported loading (DiSupLo) technique was applied for loading TER into the MSNs. The formulation was optimized by a D-optimal design, which permits the concurrent assessment of the influence of drug/MSN%, coat concentration, and MSN type on the drug entrapment efficiency (EE) and its release performance. The optimal formula displayed a high EE of 96.49%, minimizing the release in pH 1.2 to 16.15% and maximizing the release in pH 7.4 to 78.09%. The cytotoxicity of the optimal formula on the colon cancer cells HT-29 was higher than it was with TER alone by 2.8-fold. Apoptosis in cancer cells exposed to the optimum formula was boosted as compared to what it was with the plain TER by 1.2-fold and it was more efficient in arresting cells during the G0/G1 and S stages of the cell cycle. Accordingly, the repurposing of TER utilizing Eud/MSNs is a promising technique for targeted colon cancer therapy.

6.
Sensors (Basel) ; 23(20)2023 Oct 13.
Artigo em Inglês | MEDLINE | ID: mdl-37896546

RESUMO

Measurement of the intracellular pH is particularly crucial for the detection of numerous diseases, such as carcinomas, that are characterised by a low intracellular pH. Therefore, pH-responsive nanosensors have been developed by many researchers due to their ability to non-invasively detect minor changes in the pH of many biological systems without causing significant biological damage. However, the existing pH-sensitive nanosensors, such as the polyacrylamide, silica, and quantum dots-based nanosensors, require large quantities of organic solvents that could cause detrimental damage to the ecosystem. As a result, this research is aimed at developing a new generation of pH-responsive nanosensors comprising alginate natural polymers and pH-sensitive fluorophores using an organic, solvent-free, and ecologically friendly method. Herein, we successfully synthesised different models of pH-responsive alginate nanoparticles by varying the method of fluorophore conjugation. The synthesised pH nanosensors demonstrated a low MHD with a relatively acceptable PDI when using the lowest concentration of the cross-linker Ca+2 (1.25 mM). All the pH nanosensors showed negative zeta potential values, attributed to the free carboxylate groups surrounding the nanoparticles' surfaces, which support the colloidal stability of the nanosensors. The synthesised models of pH nanosensors displayed a high pH-responsiveness with various correlations between the pH measurements and the nanosensors' fluorescence signal. In summation, pH-responsive alginate nanosensors produced using organic, solvent-free, green technology could be harnessed as potential diagnostics for the intracellular and extracellular pH measurements of various biological systems.


Assuntos
Nanopartículas , Pontos Quânticos , Calibragem , Ecossistema , Concentração de Íons de Hidrogênio , Corantes Fluorescentes
7.
RSC Adv ; 13(37): 26213-26228, 2023 Aug 29.
Artigo em Inglês | MEDLINE | ID: mdl-37671007

RESUMO

In this study, Retama monosperma extract (RME) was used for the green synthesis of silver nanoparticles (RME-AgNPs). RME's phenolic profile was identified by liquid chromatography coupled to mass spectroscopy (LC-ESI/MS/MS) technique. A tentative identification of 21 phenolic metabolites from the extract was performed. The produced RME-AgNPs showed UV absorbance at 443 nm. FTIR spectroscopy confirmed the presence of RME functional groups. In addition, XRD analysis confirmed the crystallography of RME-AgNPs via exhibiting peaks with 2θ values at 38.34°, 44.29°, and 64.65°. RME-AgNPs were spherical with particle sizes ranging from 9.87 to 21.16 nm, as determined by SEM and HR-TEM techniques. The zeta potential determined the particle's charge value as -15.25 mv. RME-AgNPs exhibited significantly higher antibacterial activity against Gram-negative (Escherichia coli, Pseudomonas aeruginosa, Serratia marcescens, and Klebsiella pneumoniae) and Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) compared to RME. Moreover, the SEM images of green-synthesized nanoparticles revealed severe damage and deformation in the bacterial cell wall of the different strains subjected to the current investigation. The bioinformatics study identified 266 targets, among which only 41 targets were associated with bacterial infections. The PI3K-Akt and Relaxin signaling pathways were the top KEGG signaling pathways. Molecular docking was also performed for the 21 identified compounds at the TNF-α active site; kaempferol-3-O-robinoside-7-O-rhamnoside had a higher binding energy (-6.8084). The findings of this study warrant the use of green-synthesized AgNPs from Retama monosperma as potential antibacterial agents.

8.
Int J Gen Med ; 16: 4077-4090, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37700743

RESUMO

Objective: To investigate the knowledge, prevalence of chronic respiratory disorders, and utilization of their medications among the adults at Najran region, Saudi Arabia. Methods: An online cross-sectional survey was carried out in Najran region, Saudi Arabia. A self-administered questionnaire was distributed among a random sample of the general population, aged 18 or above between March and December 2022. The survey instrument included questions regarding history and exposure, physician diagnosed-disorders, respiratory symptoms, allergy, use of medications and possible risk-related factors. Results: This research had a total of 712 individuals. Nearly one-third of the participants in the survey (n = 218; 30.6%) said that they or a member of their family suffer from respiratory ailments. The majority of research participants (n = 167; 76.8%) identified asthma as their primary respiratory condition. A total of 32.0% of participants (n = 70) reported dealing with dust or chemicals such as paints, fertilizers, and cleaning products on a daily basis at work or at home. Around 62.0% of the participants (n = 134) said that exposure to gases, fragrances, and other such substances negatively impacts their health. Almost 78.0% (n = 169) of them indicated that summer weather affects their health, whereas 63.0% (n = 138) reported that winter cold affects their health. Participants aged 41-50 years were 38.0% less likely to have CRDs compared to others (p < 0.05). Conclusion: This study is among the first few studies that explored the knowledge, prevalence of chronic respiratory disorders, and utilization of their medications among the adults at Najran region, Saudi Arabia. In the southern area of Najran, respiratory symptoms are frequent among the inhabitants of Saudi Arabia. More research is required to discover avoidable risk factors and create countermeasures for them. It is recommended that healthcare personnel increase their efforts to educate their patients about respiratory illness prevention methods.

9.
Antibiotics (Basel) ; 12(5)2023 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-37237812

RESUMO

The nature of microorganisms and the efficiency of antimicrobials have witnessed a huge co-dependent change in their dynamics over the last few decades. On the other side, metals and metallic compounds have gained popularity owing to their effectiveness against various microbial strains. A structured search of both research and review papers was conducted via different electronic databases, such as PubMed, Bentham, Springer, and Science Direct, among others, for the present review. Along with these, marketed products, patents, and Clinicaltrials.gov were also referred to for our review. Different microbes such as bacteria, fungi, etc., and their diverse species and strains have been reviewed and found to be sensitive to metal-carrying formulations. The products are observed to restrict growth, multiplication, and biofilm formation effectively and adequately. Silver has an apt use in this area of treatment and recovery, and other metals like copper, gold, iron, and gallium have also been observed to generate antimicrobial activity. The present review identified membrane disruption, oxidative stress, and interaction with proteins and enzymes to be the primary microbicidal processes. Elaborating the action, nanoparticles and nanosystems are shown to work in our favor in well excelled and rational ways.

10.
Gels ; 9(2)2023 Feb 17.
Artigo em Inglês | MEDLINE | ID: mdl-36826332

RESUMO

The present work aimed to formulate and evaluate a polyherbal gel using Aloe barbadensis and extract of Vigna radiata for the treatment of acne, a disorder of the skin in which hair follicles and sebaceous glands are blocked, causing inflammation and redness of the skin. Aloe barbadensis pulp was collected and mixed with the extract of Vigna radiata and formulated into a gel using Carbopol 940, triethanolamine, and propylene glycol as the gelling agent, viscosity modifier, and pH modifier, respectively. The gel was evaluated for its antimicrobial properties against Staphylococcus aureus, Escherichia coli, and Candida albicans. Antimicrobial agents, such as gentamycin and fluconazole, were used as the standards. The developed formulation showed promising zone of inhibition. The gel was further evaluated for its physicochemical properties. The formulation showed a promising effect on acne together with the additive effect of Aloe barbadensis on skin.

11.
Molecules ; 28(2)2023 Jan 11.
Artigo em Inglês | MEDLINE | ID: mdl-36677806

RESUMO

Promethazine hydrochloride (PMZ), a potent H1-histamine blocker widely used to prevent motion sickness, dizziness, nausea, and vomiting, has a bitter taste. In the present study, taste masked PMZ nanocapsules (NCs) were prepared using an interfacial polycondensation technique. A one-step approach was used to expedite the synthesis of NCs made from a biocompatible and biodegradable polyamide based on l-arginine. The produced NCs had an average particle size of 193.63 ± 39.1 nm and a zeta potential of −31.7 ± 1.25 mV, indicating their stability. The NCs were characterized using differential scanning calorimetric analysis and X-ray diffraction, as well as transmission electron microscopy that demonstrated the formation of the NCs and the incorporation of PMZ within the polymer. The in vitro release study of the PMZ-loaded NCs displayed a 0.91 ± 0.02% release of PMZ after 10 min using artificial saliva as the dissolution media, indicating excellent taste masked particles. The in vivo study using mice revealed that the amount of fluid consumed by the PMZ-NCs group was significantly higher than that consumed by the free PMZ group (p < 0.05). This study confirmed that NCs using polyamides based on l-arginine and interfacial polycondensation can serve as a good platform for the effective taste masking of bitter actives.


Assuntos
Nanocápsulas , Prometazina , Camundongos , Animais , Prometazina/química , Nylons , Paladar , Percepção Gustatória , Antagonistas dos Receptores Histamínicos H1
12.
Gels ; 8(7)2022 Jul 21.
Artigo em Inglês | MEDLINE | ID: mdl-35877541

RESUMO

The present study aims to design and develop a nanoemulgel formulation of Tamoxifen citrate (TAM), a water-insoluble, potent anticancer drug, using the spontaneous emulsification method to improve topical delivery, achieve high accumulation at the tumour site, and spare the healthy tissues. The oil-based selection was related to the TAM solubility, while the surfactant and co-surfactant were chosen based on the droplets' thermodynamic stability and size. Afterwards, a pseudo-ternary phase diagram was built for the most promising formulation using two oils, olive and sesame, with a varied mix of Tween 40 as the surfactant and Trascutol HP as the co-surfactant (Smix), by the optimisation of experiments. The nanoemulsion (NE) formulations that were prepared were found to have an average droplet size of 41.77 ± 1.23 nm and 188.37 ± 3.53 nm, with suitable thermodynamic stability and physicochemical properties. Both olive and sesame oils are natural food additives due to their associated antioxidant effects; therefore, they showed no toxicity profile on breast cell lines (MCF-7, ATCC number HTB-22). The TAM-NE preparations revealed a prolonged and doublings superior cumulative percentage of in vitro release of TAM compared to TAM plain gel suspension over 24 h. The release data suggested that the Higuchi model was the best fitting kinetical model for the developed formulations of NE1, NE9, and NE18. The extended release of the drug as well as an acceptable amount of the drug permeated TAM via nanogel preparations suggested that nanoemulgel (NEG) is suitable for the topical delivery of TAM in breast cancer management. Thus, this work suggests that a nanogel of TAM can improve anticancer properties and reduce systemic adverse effects compared to a suspension preparation of TAM when applied in the treatment of breast cancer.

13.
Saudi Pharm J ; 30(4): 329-336, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35527831

RESUMO

Background: Medication error is a preventable adverse effect of medical care, whether or not it is evident or harmful to the patient. Disclosure of medication errors and improvement of patient safety are inexorably related, and they provide one of the strongest reasons to report and disclose errors, including near misses in which no harm comes to the patient. This study aimed to identify medication errors at the southern province of Saudi Arabia. Methods: A cross-sectional retrospective study was conducted by reviewing all medical records in the King Khaled Hospital in Najran, Saudi Arabia. Medication errors related information were extracted from the electronic medical system for the duration between 2018 and 2020. Results: During the study period of 2018 to 2020, a total of 4860 medication errors were identified. More than half of the reported medication errors (66.9%) were linked to ordering, prescribing, or transcribing medications. The most commonly reported medication errors connected to ordering/prescribing/transcribing were inappropriate dosage, dosage units, and therapeutic duplication of medication. The most commonly reported medication errors linked to administration were missing documentation during administration, not performing independent double-checks during the administration of high alert medications, and the administration of look-alike sound-alike (LASA) medications. The intensive care unit (ICU), female medical ward, and male medical ward were the most commonly reported locations for medication errors. Pharmacists detected more than half of the reported medication errors. Physicians were found to be responsible for 66.0% of reported medication errors, followed by nurses. Conclusion: Medication errors are common in hospital settings in Saudi Arabia's southern provinces. Efforts should be made to improve drug ordering, prescribing, and transcription in hospital settings. To guarantee optimum practices, the entire medical team should take responsibility for the patient's optimal medication administration.

14.
Pharmaceuticals (Basel) ; 15(3)2022 Mar 08.
Artigo em Inglês | MEDLINE | ID: mdl-35337119

RESUMO

One of the key challenges in developing a dry powder inhaler (DPI) of an inhalable potent fixed-dose combination (FDC) is the ability of the formulation to generate an effective and reproducible aerosol able to reach the lower parts of the lungs. Herein, a one-step approach is presented to expedite the synthesis of nanoaggregates made from a biocompatible and biodegradable polyamide based on L-lysine amino acid employing market-leading active pharmaceutical ingredients (fluticasone propionate (FP) and salmeterol xinafoate (SAL)) for the management of asthma. The nanoaggregates were synthesized using interfacial polycondensation that produced nanocapsules with an average particle size of 226.7 ± 35.3 nm and zeta potential of -30.6 ± 4.2 mV. Differential scanning calorimetric analysis and x-ray diffraction, as well as scanning electron microscopy of the produced FDC, revealed the ability of the produced nanocapsules to encapsulate the two actives and display the best aerodynamic performance. The FDC nanocapsules displayed 88.5% and 98.5% of the emitted dose for FP and SAL, respectively. The fine particle fraction of the nominated dose was superior to the marketed product (Seretide Diskus®, Brentford, United Kingdom). The in-vitro release study showed an extended drug release profile. Our findings suggest that nanoaggregates using polyamides based on L-lysine and interfacial polycondensation can serve as a good platform for pulmonary drug delivery of FDC systems.

15.
Polymers (Basel) ; 14(6)2022 Mar 08.
Artigo em Inglês | MEDLINE | ID: mdl-35335412

RESUMO

Thymoquinone (TQ), the main active constituent of Nigella sativa, has demonstrated broad-spectrum antimicrobial, antioxidant, and anti-inflammatory effects, which suggest its potential use in secondary infections caused by COVID-19. However, clinical deployment has been hindered due to its limited aqueous solubility and poor bioavailability. Therefore, a targeted delivery system to the lungs using nanotechnology is needed to overcome limitations encountered with TQ. In this project, a novel TQ-loaded poly(ester amide) based on L-arginine nanoparticles was prepared using the interfacial polycondensation method for a dry powder inhaler targeting delivery of TQ to the lungs. The nanoparticles were characterized by FTIR and NMR to confirm the structure. Transmission electron microscopy and Zetasizer results confirmed the particle diameter of 52 nm. The high-dose formulation showed the entrapment efficiency and loading capacity values of TQ to be 99.77% and 35.56%, respectively. An XRD study proved that TQ did not change its crystallinity, which was further confirmed by the DSC study. Optimized nanoparticles were evaluated for their in vitro aerodynamic performance, which demonstrated an effective delivery of 22.7-23.7% of the nominal dose into the lower parts of the lungs. The high drug-targeting potential and efficiency demonstrates the significant role of the TQ nanoparticles for potential application in COVID-19 and other respiratory conditions.

16.
Artigo em Inglês | MEDLINE | ID: mdl-35329335

RESUMO

AIMS: The diagnosis of autism spectrum disorder (ASD) is not easy as there is no direct test that exists to establish such a diagnosis. Increasing community and healthcare professional knowledge of the ASD spectrum is crucial because it will encourage parents of ASD children to seek screening and diagnosis from a specialist, allowing for better early detection and treatment. This study explored the knowledge of the general population in Saudi Arabia regarding ASD and assessed variables associated with an accurate understanding of ASD. METHODS: A total of 769 participants were involved in this cross-sectional study, which was conducted in Saudi Arabia between November 2021 and February 2022 using an online survey tool to explore the knowledge of the general population in Saudi Arabia regarding typical child development and ASD. A binary logistic regression analysis was used to determine factors affecting participants' knowledge of autism. RESULTS: Overall, the study participants showed a weak level of knowledge about autism with a mean score of 5.9 (SD: 3.1), comprising 34.7% of the total maximum obtainable score. Participants with a middle income category of 5000-7500 SR are less likely to be knowledgeable about autism compared to others (OR: 0.60 (95% CI: 0.39-0.92)) (p-value = 0.020). CONCLUSION: The participants in our study showed limited knowledge about autism. Government funds should be made available to facilitate educational services for ASD children. More funding and resources should be allocated by the government to provide assistance for children with special needs, and changes in public facilities are required to meet the demands of ASD patients. Through an informed educational effort, various media platforms should assist in improving the community's understanding of ASD and their attitude toward ASD patients. Educational campaigns should focus on enhancing the public's knowledge about ASD treatment and etiology.


Assuntos
Transtorno do Espectro Autista , Transtorno Autístico , Transtorno do Espectro Autista/diagnóstico , Transtorno do Espectro Autista/epidemiologia , Transtorno do Espectro Autista/terapia , Criança , Estudos Transversais , Conhecimentos, Atitudes e Prática em Saúde , Humanos , Arábia Saudita/epidemiologia
17.
Molecules ; 28(1)2022 Dec 30.
Artigo em Inglês | MEDLINE | ID: mdl-36615499

RESUMO

This work aimed to develop a new one-pot and readily scaled-up formulation capable of retaining 5-fluorouracil and prolonging its release to obtain a site-specific medication delivery for the potential treatment of colorectal cancer. Six polymer-based formulations were successfully produced using a thermal bulk polymerization method and loaded with 5-fluorouracil, which is a chemotherapeutic agent used in the treatment of colorectal carcinoma. The pellets produced were characterized by measuring the glass transition temperature, tensile strength, Young's modulus, and tensile elongation at break. Studies on in vitro swelling and release were carried out in phosphate-buffered saline to evaluate the behaviour of the developed system. The Young's modulus, glass transition temperature, and tensile strength all increased significantly as the crosslinker concentration increased, but the fracture strain value reduced significantly. The in vitro swelling profile of the produced formulations was significantly reduced by increasing crosslinking density. Less than 27% cumulative drug release was achieved for all formulations after 5 h of starting the release study. The highest cumulative drug release reached after 24 h was 69%. The developed drug delivery system demonstrated the ability to delay the release of 5-fluorouracil in upper gastrointestinal tract-mimicking conditions, while permitting its release in a controlled way afterward, which makes it promising for the potential delivery of 5-fluorouracil to the colon.


Assuntos
Sistemas de Liberação de Medicamentos , Fluoruracila , Implantes de Medicamento , Polímeros , Colo
18.
Gels ; 7(4)2021 Nov 14.
Artigo em Inglês | MEDLINE | ID: mdl-34842698

RESUMO

Hydrogels being a drug delivery system has great significance particularly for topical application in cutaneous open wound. Its specific physicochemical properties such as non-adhesiveness, moisture retention, exudate absorption, and gas permeability make them ideal as a drug delivery vehicle for wound healing application. Further, curcumin (a natural bioactive) was selected as a therapeutic agent to incorporate into the hydrogel system to design and develop nanogel pharmaceutical products for wound healing. Although, curcumin possesses remarkable anti-inflammatory, antioxidant, and anti-infective activity along with hastening the healing process by acting over the different stages of the wound healing process, but its poor biopharmaceutical (low aqueous solubility and skin penetrability) attributes hamper their therapeutic efficacy for skin applications. The current investigation aimed to develop the curcumin-loaded nanogel system and evaluated to check the improvement in the therapeutic efficacy of curcumin through a nanomedicine-based approach for wound healing activity in Wistar rats. The curcumin was enclosed inside the nanoemulsion system prepared through a high-energy ultrasonic emulsification technique at a minimum concentration of surfactant required to nanoemulsify the curcumin-loaded oil system (Labrafac PG) having droplet size 56.25 ± 0.69 nm with polydispersity index 0.05 ± 0.01 and negatively surface charge with zeta potential -20.26 ± 0.65 mV. It was observed that the impact of Smix (surfactant/co-surfactant mixture) ratio on droplet size of generated nanoemulsion is more pronounced at lower Smix concentration (25%) compared to the higher Smix concentration (30%). The optimized curcumin-loaded nanoemulsion was incorporated into a 0.5% Carbopol® 940 hydrogel system for topical application. The developed curcumin nanoemulgel exhibited thixotropic rheological behavior and a significant (p < 0.05) increase in skin penetrability characteristics compared to curcumin dispersed in conventional hydrogel system. The in vivo wound healing efficacy study and histological examination of healed tissue specimen further signify the role of the nanomedicine-based approach to improve the biopharmaceutical attributes of curcumin.

19.
Artigo em Inglês | MEDLINE | ID: mdl-34205637

RESUMO

AIMS: Due to the continuous changes in modern lifestyle and the need to explore the effect of these changes on the risk of developing cancer, ongoing research on the epidemiology and characteristics of cancer patients is requested. This study explored the epidemiology of cancer, its characteristics, treatment patterns, and risk factors in the southern region of Saudi Arabia. METHODS: A retrospective cross-sectional study was conducted using cancer patients' medical records at Asir Central Hospital in the southern region of Saudi Arabia. Active patients' records were extracted between January 2013 and December 2019. RESULTS: A total of 2038 patients were identified during the study period, with a mean age of 60.9 (SD: 19.0) years. The patients had survived with their cancer for a median duration of 4 years (IQR: 2-6). Around 4.6% of the patients required ICU admission with a median period of 9 days (IQR: 5-14.75). The death rate during the study period was 10.9%. Around 20.8% of the cases were metastatic, of which 77.8% were at stage four of metastasis, and 19.7% of the patients were receiving chemotherapy for their disease. The most common types of cancer were malignant neoplasms of digestive organs, comprising 40.8% of the sample. Older age (60 years and above) and using specific chronic disease medications were predictors associated with a higher risk of death due to cancer (p < 0.05). Smoking history, using specific chronic disease medications, and having previous surgery were predictors associated with a higher risk of ICU admission (p < 0.05). CONCLUSION: Breast, colon, and liver cancers were the most prevalent in the southern region of Saudi Arabia. Several modifiable cancer risk factors were identified. The results of this study should support decision-makers in the initiation of programs for key modifiable risk factors that enhance lifestyle changes and reduce cancer risks.


Assuntos
Neoplasias , Idoso , Estudos Transversais , Humanos , Pessoa de Meia-Idade , Neoplasias/epidemiologia , Neoplasias/terapia , Estudos Retrospectivos , Fatores de Risco , Arábia Saudita/epidemiologia
20.
Saudi Pharm J ; 29(5): 478-486, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-34135674

RESUMO

The delivery of antihistaminic agents via the oral route is problematic, especially for elderly patients. This study aimed to develop a sublingual formulation of promethazine hydrochloride by direct compression, and to mask its intensely bitter taste. Promethazine hydrochloride (PMZ) sublingual tablets prepared by direct compression were optimized using Box-Behnken full factorial design. The effect of a taste-masking agent (Eudragit E 100, X1), superdisintegrant (crospovidone; CPV, X2) and lubricant (sodium stearyl fumarate; SSF, X3) on sublingual tablets' attributes (responses, Y) was optimized. The prepared sublingual tablets were characterized for hardness (Y1), disintegration time (Y2), initial dissolution rate (IDR; Y3) and dissolution efficiency after 30 min (Dissolution Efficiency (DE); Y4). The obtained results showed a significant positive effect of the three independent factors on tablet hardness (P < 0.05), and the interactive effect of Eudragit E 100 and CPV on tablet hardness was significant. Disintegration time was mainly affected by Eudragit E 100 and CPV concentrations. Moreover, IDR was employed to assess the taste masking effect, lower values were obtained at higher Eudragit E 100 concentration despite it was statistically insignificant (p > 0.05). Optimized formulation that was suggested by the software was composed of: Eudragit E 100 (X1) = 2.5% w/w, CPV (X2) = 4.13% w/w, and SSF (X3) = 1.0% w/w. The observed values of the optimized formula were found to be close to the predicted optimized values. The Differential Scanning Calorimetric (DSC) studies indicated no interaction between PMZ and tablet excipients.

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